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Purity: ≥98%
Reparixin (also known as Repertaxin), is a novel, potent small molecular weight allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. It is the first medication candidate that is being studied in a clinical setting to prevent ischemia/reperfusion damage in organ transplant recipients. Dual allosteric CXCR1 and CXCR2 inhibitors have been designed using a computer-aided design program that took into account the mode of binding of reparixin to CXCR1. A noncompetitive allosteric mode of interaction between CXCR1 and Repertaxin, which stops signaling by locking CXCR1 in an inactive conformation, is consistent with structural and biochemical data. Repertaxin shields organs from reperfusion injury and is an efficient in vivo inhibitor of polymorphonuclear cell recruitment. One general tactic to alter chemoattractant receptor activity is to target the Repertaxin interaction site of CXCR1.
| Targets |
CXCR1wt ( IC50 = 5.6 nM ); CXCR1Ile43Val ( IC50 = 80 nM ); CXCR1 ( IC50 = 1 nM ); CXCR2 ( IC50 ∼100 nM )
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| Enzyme Assay |
Reparixin L-lysine salt is a new and powerful small molecular weight allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. It is the L-lysine salt form of reparixin. Reparixin, as demonstrated in particular experiments on CXCR1/L1.2 and CXCR2/L1.2 transfected cells and on human PMNs, is a strong functional inhibitor of CXCL8-induced biological activities on human PMNs with a marked selectivity (about 400-fold) for CXCR1. Reparixin's effectiveness is considerably reduced in L1.2 cells that express the CXCR1 Ile43Val mutant (IC50 values for CXCR1 wt and CXCR1 Ile43Val, respectively, are 5.6 nM and 80 nM).
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| Cell Assay |
L1.2 Cell suspension (1.5-3×106 cells/mL) is then seeded in triplicate in the upper compartment of the chemotactic chamber after being incubated for 15 min at 37°C with either vehicle or Reparixin (1 nM-1μM). The following concentrations of various agonists are seeded in the chamber's lower compartment: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, and 30 nM C5a. The chemotactic chamber is incubated for 45 minutes (human PMNs) or 2 hours (monocytes) at 37°C in air with 5% CO2. After the incubation period, the filter is taken out, cleaned, and stained. Five oil immersion fields are counted for each migration at a high magnification of 100×, following sample coding. Transwell filters with a pore size of 5 μm are used to assess L1.2 migration.
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| References |
| Molecular Formula |
C14H21NO3S
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| Molecular Weight |
283.39
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| Exact Mass |
283.12
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| Elemental Analysis |
C, 59.34; H, 7.47; N, 4.94; O, 16.94; S, 11.31
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| CAS # |
266359-83-5
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| Related CAS # |
(Rac)-Reparixin; 957407-64-6; Reparixin L-lysine salt; 266359-93-7
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| Appearance |
Solid powder
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| SMILES |
C[C@H](C1=CC=C(C=C1)CC(C)C)C(=O)NS(=O)(=O)C
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| InChi Key |
KQDRVXQXKZXMHP-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C14H21NO3S/c1-10(2)9-12-5-7-13(8-6-12)11(3)14(16)15-19(4,17)18/h5-8,10-11H,9H2,1-4H3,(H,15,16)/t11-/m1/s1
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| Chemical Name |
(2R)-2-[4-(2-methylpropyl)phenyl]-N-methylsulfonylpropanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: 2.5 mg/mL (8.82 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5287 mL | 17.6435 mL | 35.2871 mL | |
| 5 mM | 0.7057 mL | 3.5287 mL | 7.0574 mL | |
| 10 mM | 0.3529 mL | 1.7644 mL | 3.5287 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05496868 | Recruiting | Drug: Reparixin 600mg Other: Matching Placebo |
Acute Respiratory Distress Syndrome, Adult |
Dompé Farmaceutici S.p.A | February 7, 2023 | Phase 2 |
| NCT05254990 | Recruiting | Drug: Reparixin Other: Placebo |
Infectious Pneumonia Severe COVID-19 |
Dompé Farmaceutici S.p.A | April 6, 2022 | Phase 3 |
| NCT05835466 | Recruiting | Drug: reparixin | Myelofibrosis (PMF) Post Essential Thrombocythemia Myelofibrosis (ET-MF) |
Icahn School of Medicine at Mount Sinai |
June 27, 2023 | Phase 2 |
| NCT04878055 | Completed | Drug: Reparixin Other: Placebo |
Pneumonia, Viral | Dompé Farmaceutici S.p.A | February 14, 2021 | Phase 3 |
| NCT02370238 | Completed | Drug: paclitaxel Drug: Reparixin |
Metastatic Breast Cancer | Dompé Farmaceutici S.p.A | July 29, 2015 | Phase 2 |
 Effect of Repertaxin on CXCL8 activity and binding to cellular receptors.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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 Effect of Repertaxin on cell signaling activated by CXCL8.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
 In vivoefficacy of Repertaxin in inhibiting PMN recruitment in CLP.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
 Molecular modeling of Repertaxin interaction with CXCR1/CXCR2.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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 In vivoefficacy of Repertaxin in inhibiting PMN recruitment and tissue damage in RI.Proc Natl Acad Sci U S A.2004 Aug 10;101(32):11791-6. |
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